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ChEMBL ligand: CHEMBL374975 (Acide fusidique, Acido fusidico, Anhydrous fusidic acid, CEM-102, Fucidin caviject, Fucithalmic, Fusidate, Fusidic acid, NSC-56192, Ramycin, SQ 16,603, SQ-16603, Taksta) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in dog MDCK-II-BCRP cells incubated for 120 mins by transwell migration assay | B | 4.28 | pIC50 | 52000 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
ChEMBL | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.94 | pIC50 | 11500 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Taurocholate uptake in canalicular membrane vesicles of rat liver | F | 5.66 | pKi | 2200 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.76 | pIC50 | 17400 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of LTC4 uptake in Mrp2-expressing HEK cells | F | 4.89 | pKi | 13000 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
ChEMBL | TP_TRANSPORTER: inhibition of E217betaG uptake in canalicular membrane vesicles of rat liver | F | 5.12 | pKi | 7600 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
ChEMBL | TP_TRANSPORTER: inhibition of LTC4 uptake in canalicular membrane vesicles of rat liver | F | 5.26 | pKi | 5500 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay | F | 4.23 | pIC50 | 59000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840] |
ChEMBL | Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 infected in human RBC after 48 hrs by [3H]hypoxanthine incorporation assay | F | 4.23 | pIC50 | 59000 | nM | IC50 | Medchemcomm (2015) 6: 2023-2028 |
ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting | F | 4.23 | pIC50 | 59000 | nM | IC50 | Medchemcomm (2017) 8: 1152-1157 [PMID:30108825] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 infected in human RBC after 48 to 96 hrs by SYBR Green I dye-based fluorescence assay | F | 4.28 | pIC50 | 52800 | nM | IC50 | Medchemcomm (2015) 6: 2023-2028 |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 48 hrs | F | 4.28 | pIC50 | 52800 | nM | IC50 | Medchemcomm (2017) 8: 1152-1157 [PMID:30108825] |
ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes after 48 hrs by giemsa staining based assay | F | 4.3 | pIC50 | 50000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840] |
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay | F | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]